scholarly journals Pulsatile Delivery of Fexofenadine Hydrochloride Pulsincap by Box-Behnken Design

2021 ◽  
pp. 649-663
Author(s):  
D. Prasanthi ◽  
Shreya Ajay Rajguru ◽  
C. Aishwarya ◽  
Aisha Rahman
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Early Morning ◽  
Box Behnken Design ◽  
Dsc Studies ◽  
Physico Chemical ◽  
Dependent Variables ◽  
Contour Plots ◽  
Pulsatile Delivery ◽  
Polymer Ratio

Objective: Fexofenadine hydrochloride is a selective peripheral H1-blocker, used for allergy symptoms, such as hay fever and urticaria. Allergic symptoms are aggressive during early morning hours, so a pulsatile delivery system with a lag time of 4-5 hours was formulated and optimized by Box-Behnken design. Materials and Methods: Pulsincap system using formaldehyde-treated capsules and hydrogel plug.  Box-Behnken design was applied for optimization in which three independent variables, X1= Drug: polymer ratio, X2 = Polymer: polymer ratio (Ethylcellulose: HPMC E15) and X3 = Plug weight were selected. Three dependent variables R1 = Percent release of drug after 4 hours, R2 = percent release after 10 hours and R3 = Lag time were selected. Results: FTIR and DSC studies confirmed compatibility of drug and excipients. The empty formaldehyde-treated capsules were evaluated for physical appearance, solubility, capsule dimensions and formaldehyde content. Hydrogel plugs, powder blend and pulsincap formulations were evaluated for Physico-chemical parameters and all the parameters were within acceptable limits. Contour plots and Response surface plots indicated that as Drug: Polymer ratio (X1) and Plug weight (X3) increased, Lag time increased but% drug release decreased. As Polymer: Polymer ratio (X2) increased, the lag time was at a moderate level. Predicted vs actual responses showed the correlation of 0.786 for% release in 4hrs, 0.9744 for% release in 10hrs and 0.6281 for lag time. Optimized formulation G1 was suggested by design (with criteria 4.5-6hrs lag time, 10-20% release in 4hrs & 60-70% drug release within 10hrs). The optimised formulation was stable. Conclusion: Pulsincap system of Fexofenadine hydrochloride can be obtained by using retarding polymers like ethyl cellulose, HPMC E15 and formaldehyde cross-linked capsules.

scholarly journals Development and Optimization of Acyclovir Loaded Mucoadhesive Microspheres by Box – Behnken Design

2019 ◽  
Vol 18 (1) ◽  
pp. 1-12
Author(s):  
James Regun Karmoker ◽  
Ikramul Hasan ◽  
Nusrat Ahmed ◽  
Mohammad Saifuddin ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Response Surface ◽  
Drug Release Profile ◽  
Box Behnken Design ◽  
Dependent Variables ◽  
Contour Plots ◽  
Evaporation Technique ◽  
Predicted Values ◽  
Emulsification Solvent Evaporation ◽  
Experimental Values

The grail of the study was to design, develop and characterize sustained release mucoadhesive microspheres of acyclovir and to optimize the drug release profile using response surface methodology by applying Box–Behnken design (BBD) which was equipped with three levels and three factors. Microspheres were prepared from Methocel K15M and Ethocel Standard 45 Premium using the emulsification solvent evaporation technique. The independent factors were the amounts of Methocel K15M (X1), amount of Ethocel Standard 45 Premium (X2), and RPM (X3). The dependent variables were cumulative percentage drug release (CDR) at 8 hour (Y1), bond strength (Y2), and swelling at 4 hour (Y3). To understand the effects of different factor level combinations on the responses, various response surface graphs and contour plots were prepared. Predicted values and experimental values for optimized formulation (X1 = 600 mg, X2 = 500 mg, and X3 = 336.57) was found to be in close agreement. Dhaka Univ. J. Pharm. Sci. 18(1): 1-2, 2019 (June)

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

scholarly journals DESIGN AND STATISTICAL EVALUATION OF A MULTIUNIT DELIVERY SYSTEM CONTAINING NISOLDIPINE-SOLUPLUS® SOLID DISPERSION FOR HYPERTENSION CHRONOTHERAPY

2016 ◽  
Vol 8 (10) ◽  
pp. 170
Author(s):  
Sandeep Kumar Vats ◽  
Roop Narayan Gupta ◽  
Kalaiselvan Ramaraju ◽  
Romi Singh
Keyword(s):  
Drug Release ◽  
Response Surface ◽  
Solid Dispersion ◽  
Lag Time ◽  
Core Level ◽  
Factors Affecting ◽  
Eudragit S100 ◽  
Inert Core ◽  
Dissolution Efficiency ◽  
Polymer Ratio

<p><strong>Objective: </strong>To study the mechanism and factors affecting the design of an industrially scalable formulation in a combined drug delivery module containing solid dispersion (SD) multiunit pellets with novel polymer Soluplus® in a modified release system to address chronotherapeutic needs of hypertension therapy.</p><p><strong>Methods: </strong>Nisoldipine-Soluplus® SD pellet formulations were prepared using the central composite design of experiments (CCD) to study the effect of inert core level and drug to polymer ratio. The solid dispersions were formed on inert pellets surface by fluidized bed coating and characterized by dissolution efficiency and time for 90% drug release. The data was statistically analyzed to develop a response surface for optimum SD formulation in pellets. The SD pellets were characterized by FTIR, DSC and SEM. The optimum formulation of SD coated pellets was further coated with Eudragit S100-L100 polymer mix and characterized for dissolution in multimedia and two-step dissolution for lag time.</p><p><strong>Results: </strong>A response surface was developed for highest dissolution efficiency (%DE) and least time to release 90% drug (T<sub>90</sub>). The model was significant, and the role of core pellets was found to be more significant than the drug-polymer ratio. The study of the desirability function indicated that a polymer content of 75% and inert core level to yield 23% net weight gain, provided optimum dissolution enhanced SD pellets. The drug was found to exist in amorphous form. The final capsules containing Eudragit S100-L100 coated delayed release SD pellets showed a lag time of 2 h and a definite pH-gradient towards drug release.</p><p><strong>Conclusion: </strong>The findings from this study helped to understand the mechanism, design and factors affecting drug release from a delayed release SD system for a poorly soluble drug for potential hypertension chronotherapy.</p>

scholarly journals Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, andIn VitroandIn VivoEvaluation

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Gagganapalli Santhoshi Reddy ◽  
Usha Yogendra Nayak ◽  
Praful Balavant Deshpande ◽  
Srinivas Mutalik
Keyword(s):  
Blood Pressure ◽  
Drug Release ◽  
Immediate Release ◽  
Lag Time ◽  
Early Morning ◽  
Quadratic Model ◽  
Pharmacokinetic Parameters ◽  
Pulsatile Release

The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat early morning surge in blood pressure. Immediate release core tablets containing lercanidipine HCl were prepared and optimized core tablets were compression-coated using buoyant layer containing polyethylene oxide (PEO) WSR coagulant, sodium bicarbonate, and directly compressible lactose. FPRTs were evaluated for variousin vitrophysicochemical parameters, drug-excipient compatibility, buoyancy, swelling, and release studies. The optimized FPRTs were testedin vivoin New Zealand white rabbits for buoyancy and pharmacokinetics. DoE optimization of data revealed FPRTs containing PEO (20% w/w) with coat weight 480 mg were promising systems exhibiting good floating behavior and lag time in drug release. Abdominal X-ray imaging of rabbits after oral administration of the tablets, confirmed the floating behavior and lag time. A quadratic model was suggested for release at 7th and 12th h and a linear model was suggested for release lag time. The FPRT formulation improved pharmacokinetic parameters compared to immediate release tablet formulation in terms of extent of absorption in rabbits. As the formulation showed delay in drug release bothin vitroandin vivo, nighttime administration could be beneficial to reduce the cardiovascular complications due to early morning surge in blood pressure.

Design, Development and Optimization of Pulsatile Core in Cup Tablets of Naproxen

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Rutu H. Patel ◽  
ImadHadi Hameed ◽  
Kunal N. Patel ◽  
Madhabhai M. Patel
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Major Effect ◽  
Stability Study ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
Accelerated Stability ◽  
Excipient Compatibility

The aim of the present study to prepare Pulsatile release tablet of naproxen for the treatment of rheumatoid arthritis. The drug delivery system was designed to deliver the drug at a time when it could be most needful for the patient. Drug excipient compatibility studies were carried out using DSC and found to be compatible with each other. Pulsatile tablet was prepared by direct compression method using different type and amount of superdisintegrants and coating polymers and evaluated for pre and post compression parameters. Box Behnken design was applied to optimize responses. Concentrations of Sodium starch glycolate (SSG) (X1), Ethyl cellulose (EC) (X2), and HPMC K100M (X3) were selected as independent variables while Lag time (Y1) and % drug release at 8 hrs (Y2) were selected as dependent variables. The prepared tablets were evaluated for post compression parameters and results indicated that concentration of SSG has major effect on in vitro drug release while concentration of EC and HPMC K100M has major effect on Lag time. Batch BE13 prepared with SSG 35mg, EC 175mg, and HPMC K100M 75 mg was found to be best batch as it achieves predetermined lag time of 5 hr 02 min and 99.32% of drug release. There was no significant variation in formulation at the end of six month accelerated stability study.

scholarly journals Formulation and evaluation of compression Coated tablets of Lornoxicam for Targeting early morning peak symptoms of Rheumatoid arthritis

2014 ◽  
Vol 12 (2) ◽  
pp. 109-117 ◽  
Author(s):  
Mohd Abdul Hadi ◽  
NG Raghavendra Rao ◽  
A Srinivasa Rao
Keyword(s):  
Rheumatoid Arthritis ◽  
Research Work ◽  
Lag Time ◽  
Early Morning ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
The Core ◽  
Ich Guidelines

In the present research work, we have designed a pulsatile formulation of lornoxicam to treat rheumatoid arthritis as per the chronotherapeutic pattern of the disease. Core tablets were prepared by incorporating different concentration of disintegrants and were compressed in between different concentration and combination of hydrophobic and hydrophilic polymers. The core and compression coated tablets were subjected to pre-formulation, physicochemical, in-vitro drug release and stability studies. FTIR and DSC studies revealed that there was not any chemical reaction between pure drug lornoxicam and polymers. The pre and post-compressional parameters of tablets were also found to be within limits. The core tablets which were incorporated with 10% of crospovidone were found to be as most fastly disintegrating. Our optimized formulation F-5 releases lornoxicam after a lag time of 5.5±0.7 hours and 99.81±0.81% upto 8 hours. Stability was also found for the optimized formulation according to ICH guidelines. Dhaka Univ. J. Pharm. Sci. 12(2): 109-117, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17620

scholarly journals Preparation and evaluation of matrix type gastro retentive floating atenolol tablets using sintering technique.

2020 ◽  
Vol 11 (2) ◽  
pp. 1920-1926
Author(s):  
Munagala Gayatri Ramya ◽  
Kothapalli Bannoth Chandra Sekhar
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Lag Time ◽  
Content Uniformity ◽  
Floating Tablets ◽  
Dsc Studies ◽  
Weight Variation ◽  
Different Temperatures ◽  
Thermal Sintering ◽  
Gastro Retentive

The aim of this investigation was to design and assess the gastric floating tablets of Atenolol using thermal sintering and investigate the effect of sintering on PEO polymer. Atenolol is an Antihypertensive with only 50 percent bioavailability due to poor absorption in lower GI tract. Gastro retentive Floating tablets were prepared to enhance the gastric retention time, to prolong the drug release. PEO which was selected as sintered polymer. Tablets were prepared by direct compression method .Formulated tablets were exposed to different temperatures (400C, 500C and 600C)  at various time intervals( 1h ,2h ,3h and4h) in a hot air oven .Post compression parameters were evaluated like weight variation, hardness, friability, floating lag time and total floating time. The result of the investigation indicates sintering influenced the floating time and dissolution properties. Weight variation, friability and content uniformity values were within limits. Sintering time and temperature contributes to effectiveness of polymers in extending drug release. Reduction in floating lag time and increase in total floating time as well as release of drug was delayed. All sintered formulation have no interaction was found in FTIR, DSC studies. All sintered tablets followed zero order with nonfickian diffusion mechanism. This study helps the use of thermal sintering in preparation of floating tablets.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST

2021 ◽  
pp. 211-220
Author(s):  
N. SHIVA KRISHNA ◽  
B. JAYANTHI ◽  
A. MADHUKAR
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Early Morning ◽  
Release Profile ◽  
Locust Bean Gum ◽  
In Vitro Drug Release ◽  
The Core ◽  
Locust Bean ◽  
Core Tablet

Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning. Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids. Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo. Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

scholarly journals Formulation and Evaluation of Bio-adhesive Pulsatile Drug Delivery System of Telmisartan

2020 ◽  
Vol 11 (2) ◽  
pp. 1282-1287
Author(s):  
Patil S. V. ◽  
Salokhe P. A. ◽  
Patil S. S. ◽  
Ustad J. Y. ◽  
Shedbale S. S.
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Early Morning ◽  
Pulsatile Drug Delivery ◽  
Hypertensive Drug ◽  
Time Specific ◽  
Core Tablet

The main objective of this study was to formulate and evaluate of Bio-adhesive pulsatile drug delivery system of Telmisartan, an anti-hypertensive drug in order to achieve better therapeutic efficacy and patient compliance. The approach of combination of bio-adhesive pulsatile formulation is suitable for gastro retention and time specific drug delivery. The study was carried by preparation of fast disintegrating core tablet followed by incorporation of core tablet to design bio-adhesive pulsatile tablet by press coating. The press coated tablet was prepared with the polymersethyl cellulose and carbopol. The formulation was evaluated for precompression and post compression parameters, lag time, drug release and bio-adhesive study. All evaluation parameters were found within limits. The lag time expected for this disease was 8 hours as need of drug release for this disease was more likely to act in early morning. The 8 hour lag time was obtained in optimized formulation which has shown muco-adhesion for the same period. Thus bio-adhesive pulsatile drug delivery system could be the best precautionary alternative for the drugs having maximum absorption in stomach and used for diseases which follows circadian rhythm.

Trimetazidine Dihydrochloride Pulsatile–Release Tablets for the Treatment of Morning Anginal Symptoms: Dual Optimization, Characterization and Pharmacokinetic Evaluation

2021 ◽  
Vol 18 ◽  
Author(s):  
Abdelrahman I. Othman ◽  
Maha M. Amin ◽  
Sherif K. Abu-Elyazid ◽  
Ghada A. Abdelbary
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Chronic Stable Angina ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Relative Bioavailability ◽  
Early Morning ◽  
Stability Study ◽  
Disintegration Time ◽  
Pulsatile Release

Objective: This research work aimed to target the early morning peak symptoms of chronic stable angina through formulating antianginal drug, Trimetazidine (TMZ) in a pulsatile-release tablet. Methods: The core formulae were optimized using 22.31 factorial design to minimize disintegration time (DT) and maximize drug release after 5 minutes (Q5min). Different ratios of Eudragit S100 and Eudragit L100 were used as a coating mixture for the selected core with or without a second coating layer of hydroxypropyl methyl cellulose (HPMC E50). The different formulation variables were statistically optimized for their effect on lag time and drug release after 7 hours (Q7h) using Box-Behnken design. The optimized formula (PO) was subjected to stability study and pharmacokinetic assessment on New Zealand rabbits. Results: The optimal core (F8) was found to have 1.76 min disintegration time and 61.45% Q5min PO showed a lag time of 6.17 h with 94.80% Q7h and retained good stability over three months. The pharmacokinetic study confirmed the pulsatile–release pattern with Cmax of 206.19 ng/ml at 5.33 h (Tmax), as well as 95.85% relative bioavailability compared to TMZ solution. Conclusion: Overall pulsatile-release tablets of TMZ succeeded in releasing the drug rapidly after a desirable lag time, providing a promising approach for early morning anginal symptoms relief.

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